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Selleckchem/SD 0006/S6502

DescriptionSD0006isaninhibitorofp38kinase-alpha(p38alpha)withIC50valuesof0.016μMand0.677μMforp38αandp38β.Itisselectiveforp38αkinaseover50otherkinasesscreened(includingp38γandp38δwithmodestselectivityoverp38β).
Targets
p38α[1](Cell-freeassay)p38β[1](Cell-freeassay)
0.016μM0.677μM
Invitro

SD0006isselectiveforp38αkinaseover50otherkinasesscreened(includingp38γandp38δwithmodestselectivityoverp38β).ItsuppressesInflammatorymediatorreleaseincellularstudies.SD0006suppressesexpressionofmultipleproinflammatoryproteinsatboththetranscriptionalandtranslationallevels.InRASFs,SD0006hasnodirectinhibitoryactivityagainstCOX-1orCOX-2,yetitcouldcompletelyinhibitinadose-dependentmannerthereleaseofIL-1β-stimulatedPGE2withanIC50of96.2nmol/l[1].

Invivo

Invivo,SD0006iseffectiveinanimalmodelsofchronicinflammationanddisease.Itiseffectiveintheratstreptococcal-cell-wall-inducedarthritismodel,withdramaticprotectiveeffectsonpawjointintegrityandbonedensity.SD0006alsodemonstratesgoodoralanti-inflammatoryefficacywithexcellentcross-speciescorrelationbetweentherat,cynomolgusmonkey,andhuman.Italleviatesswellingandpaininarodentacuteinflammationmodel[1].

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